Speed and Accuracy of Recording Medication History by Pharmacists in Secondary Emergency Rooms.

In Japan, only few hospitals have pharmacists in their secondary emergency rooms to record medication history and provide drug information in real time. In this study, we investigated the benefits of pharmacist intervention in secondary emergency rooms by comparing the time taken by the pharmacists and non-pharmacists in the emergency room to record the medication history in the electronic medical record and the accuracy of its content. The study period was from September 1 to September 30, 2022, and included patients who were transported to our hospital for emergency care between 9:00 and 16:30. We compared the time taken between the patient's arrival until the recording of their medication history and the accuracy of the record by the emergency room pharmacists and non-pharmacists (paramedics or medical clerks). The study included 58 patients whose medication histories were collected by pharmacists, and 11 patients whose histories were collected by non-pharmacists. For pharmacists, the median time to record medication history in the electronic medical record was 12 min, whereas for non-pharmacists, it was 19 min, which was significantly different (p=0.015). The pharmacists accurately recorded the medication history of 98.3% (57/58) of patients, whereas non-pharmacists accurately recorded it for only 54.5% (6/11) of patients, with a significant difference (p<0.01). We observed that in secondary emergency rooms, when pharmacists were responsible for recording the patients' medication histories, it resulted in rapid and accurate sharing of medication history.

Synthesis and Evaluation of a Cathepsin B-Recognizing Trifunctional Chelating Agent to Improve Tumor Retention of Radioimmunoconjugates.

Cathepsin B (CTSB) is a lysosomal protease that is overexpressed in tumor cells. Radioimmunoconjugates (RICs) composed of CTSB-recognizing chelating agents are expected to increase the molecular weights of their radiometabolites by forming conjugates with CTSB in cells, resulting in their improved retention in tumor cells. We designed a novel CTSB-recognizing trifunctional chelating agent, azide-[111In]In-DOTA-CTSB-substrate ([111In]In-ADCS), to synthesize a RIC, trastuzumab-[111In]In-ADCS ([111In]In-TADCS), and evaluated its utility to improve tumor retention of the RIC. [111In]In-ADCS and [111In]In-TADCS were synthesized with satisfactory yield and purity. [111In]In-ADCS was markedly stable in murine plasma until 96 h postincubation. [111In]In-ADCS showed binding to CTSB in vitro, and the conjugation was blocked by the addition of CTSB inhibitor. In the internalization assay, [111In]In-TADCS exhibited high-level retention in SK-OV-3 cells, indicating the in vitro utility of the CTSB-recognizing unit. In the biodistribution assay, [111In]In-TADCS showed high-level tumor accumulation, but the retention was hardly improved. In the first attempt to combine a CTSB-recognizing unit and RIC, these findings show the fundamental properties of the CTSB-recognizing trifunctional chelating agent to improve tumor retention of RICs.

Reproducibility and Validity of the Kerlan-Jobe Orthopedic Clinic Shoulder and Elbow Score (Japanese Version).

BACKGROUND: The Kerlan-Jobe Orthopedic Clinic (KJOC) questionnaire is a self-reported performance and functional assessment tool with good reliability and validity for overhead athletes with shoulder and elbow injuries. This study aimed to develop a Japanese version of the KJOC (J-KJOC) to clarify its reproducibility and validity for use by Japanese university baseball players. METHODS: The J-KJOC was translated according to the guidelines for cross-cultural adaptation. A total of 88 university baseball players completed the J-KJOC and the Quick-Disabilities of the Arm, Shoulder, and Hand (Q-DASH) questionnaires. Thirty players completed the J-KJOC two times after a median interval of two weeks. We assessed the absolute reliability, construct validity, internal consistency, and test-retest reliability. RESULTS: Cronbach's alpha coefficients ranged from 0.88 and the intraclass correlation coefficient for the total score was 0.91. A fixed bias was absent in the J-KJOC scores (mean difference: -2.2, 95% CI: -4.8 to 0.5). Furthermore, the J-KJOC score was correlated with the Q-DASH-disability/symptom (r = -0.60, p<0.01) and Q-DASH-sports/music (r = -0.63, p<0.01) scores but not correlated with the Q-DASH-work score (r = -0.11, p = 0.316). CONCLUSIONS: The J-KJOC questionnaire demonstrated good reproducibility and validity for assessing upper arm performance in Japanese university baseball players. The results of this study support the use of the J-KJOC for Japanese-speaking baseball players. Further research using this instrument on other types of overhead athletes is needed to determine its wider utility in sports medicine applications.

Development of Novel Bimodal Agents Based on Near-Infrared BODIPY-Conjugated Hoechst Derivatives for Combined Use in Auger Electron and Photodynamic Cancer Therapy.

Auger electron therapy and photodynamic therapy (PDT) have attracted attention as powerful anticancer modalities. Herein, we report the development of novel bimodal agents for Auger electron therapy and PDT, and their application to combination therapy. [125I]NBH-1/NBH-1 and [125I]NBH-2/NBH-2, composing Hoechst and iodostyryl-BODIPY, were synthesized and evaluated regarding their usefulness as bimodal agents. [125I]NBH-1 showed significantly higher nuclear uptake than [125I]NBH-2 and radioactivity-dependent cytotoxicity induced by Auger electrons. In addition, NBH-1 exhibited photoinduced cytotoxicity. Combination therapy using [125I]NBH-1 and NBH-1 with light irradiation induced a superior cytotoxicity to these treatments alone. In tumor-bearing mice injected with NBH-1 or [125I]NBH-1/NBH-1 under light irradiation, significant tumor growth inhibition was observed compared with that of the control group. Especially, [125I]NBH-1/NBH-1 under light irradiation showed the strongest therapeutic effects among all treatments. These results suggest that [125I]NBH-1/NBH-1 is a potent bimodal agent for Auger therapy and PDT and that combination therapy using [125I]NBH-1 and NBH-1 shows enhanced therapeutic efficacy.

Potential Role of Pig UCP3 in Modulating Adipocyte Browning via the Beta-Adrenergic Receptor Signaling Pathway.

Adipose tissue plays an important role in regulating body temperature and metabolism, with white adipocytes serving as storage units for energy. Recent research focused on the browning of white adipocytes (beige adipocytes), causing thermogenesis and lipolysis. The process of browning is linked to the activation of uncoupling protein (UCP) expression, which can be mediated by the ß3 adrenergic receptor pathway. Transcriptional factors, such as peroxisome proliferator activated receptor γ (PPARγ) and PPARγ coactivator 1 alpha, play vital roles in cell fate determination for fat cells. Beige adipocytes have metabolic therapeutic potential to combat diseases such as obesity, diabetes mellitus, and dyslipidemia, owing to their significant impact on metabolic functions. However, the molecular mechanisms that cause the induction of browning are unclear. Therefore, research using animal models and primary culture is essential to provide an understanding of browning for further application in human metabolic studies. Pigs have physiological similarities to humans; hence, they are valuable models for research on adipose tissue. This study demonstrates the browning potential of pig white adipocytes through primary culture experiments. The results show that upregulation of UCP3 gene expression and fragmentation of lipid droplets into smaller particles occur due to isoproterenol stimulation, which activates beta-adrenergic receptor signaling. Furthermore, PPARγ and PGC-1α were found to activate the UCP3 promoter region, similar to that of UCP1. These findings suggest that pigs undergo metabolic changes that induce browning in white adipocytes, providing a promising approach for metabolic research with potential implications for human health. This study offers valuable insights into the mechanism of adipocyte browning using pig primary culture that can enhance our understanding of human metabolism, leading to cures for commonly occurring diseases.

[A Questionnaire Survey of Nurses on Pharmacist Services in the Emergency Rooms at Tokushukai Medical Group].

We conducted a multicenter survey of emergency room nurses to obtain information that would be useful for the establishment of pharmacist services in emergency rooms. Notably, 199 valid responses were obtained from 12 hospitals. The most common expectation from pharmacists in the emergency room was "drug management" (70.9%), followed by "providing information to physicians regarding the patient's medication history" (59.3%), and "auditing of dosage and interaction" (57.3%). The working arrangements that the survey respondents wanted regarding pharmacists in emergency rooms were: 24 h pharmacist (41.7% wanted this arrangement), day-shift pharmacist (24.6% wanted this arrangement), 24 h on-call (17.1% wanted this arrangement), day-shift on-call (5.0% wanted this arrangement), telephone support (11.1% wanted this arrangement), and 0.5% said that there was no need for pharmacists. In the analysis of factors affecting nurse satisfaction, day-shift pharmacist was a significant factor. We hope that the results of this survey will be used as a guide for the development of emergency room pharmacist services tailored to the unique characteristics and actual working conditions of each hospital.

Development of Triphenylmethane Dyes for In Vivo Fluorescence Imaging of Aß Oligomers.

Detection of amyloid ß (Aß) oligomers, regarded as the most toxic aggregated forms of Aß, can contribute to the diagnosis and treatment of Alzheimer's disease (AD). Thus, the development of imaging probes for in vivo visualization of Aß oligomers is crucial. However, the structural uncertainty regarding Aß oligomers makes it difficult to design imaging probes with high sensitivity to Aß oligomers against highly aggregated Aß fibrils. In this study, we developed Aß oligomer-selective fluorescent probes based on triphenylmethane dyes through screening of commercially available compounds followed by structure-activity relationship (SAR) studies on cyclic or acyclic 4-dialkylamino groups. We synthesized 11 triarylmethane-based Aß oligomer probe (TAMAOP) derivatives. In vitro evaluation of fluorescence properties, TAMAOP-9, which had bulky 4-diisobutylamino groups introduced into three benzenes of a twisted triphenylmethane backbone, showed marked fluorescence enhancement in the presence of Aß oligomers and demonstrated high selectivity for Aß oligomers against Aß fibrils. In docking studies using the Aß trimer model, TAMAOP-9 bound to the hydrophobic surface and interacted with the side chain of Phe20. In vitro section staining revealed that TAMAOP-9 could visualize Aß oligomers in the brains of AD model mice. An in vivo fluorescence imaging study using TAMAOP-9 showed significantly higher fluorescence signals from the brains of AD model mice than those of age-matched wild-type mice, confirmed by ex vivo section observation. These results suggest that TAMAOP-9 is a promising Aß oligomer-targeting fluorescent probe applicable to in vivo imaging.

Fundamental evaluation regarding the relationship between albumin-binding and tumor accumulation of PSMA-targeting radioligands.

OBJECTIVE: The marked success of prostate-specific membrane antigen (PSMA)-targeting radioligands with albumin binder (ALB) is attributed to the improvement of blood retention and tumor accumulation. [111In]In-PNT-DA1, our PSMA-targeting radioligand with ALB, also achieved improved tumor accumulation due to its prolonged blood retention. Although the advantage of ALBs is related to their reversible binding to albumin, the relationship between albumin-binding and tumor accumulation of PSMA-targeting radioligands remains unclear because of the lack of information about radioligands with stronger albumin-binding than ALBs. In this study, we designed and synthesized [111In]In-PNT-DM-HSA, a new radioligand that consists of a PSMA-targeting radioligand covalently bound to albumin. The pharmacokinetics of [111In]In-PNT-DM-HSA was compared with those of [111In]In-PNT-DA1 and [111In]In-PSMA-617, a non-ALB-conjugated radioligand, to evaluate the relationship between albumin-binding and tumor accumulation. METHOD: The [111In]In-PNT-DM-HSA was prepared by incubation of [111In]In-PNT-DM, a PSMA-targeting radioligand including a maleimide group, and human serum albumin (HSA). The ability of [111In]In-PNT-DM-HSA was evaluated by in vitro assays. A biodistribution study using LNCaP tumor-bearing mice was conducted to compare the pharmacokinetics of [111In]In-PNT-DM-HSA, [111In]In-PNT-DA1, and [111In]In-PSMA-617. RESULTS: The [111In]In-PNT-DM-HSA was obtained at a favorable radiochemical yield and high radiochemical purity. In vitro assays revealed that [111In]In-PNT-DM-HSA had fundamental characteristics as a PSMA-targeting radioligand interacting with albumin covalently. In a biodistribution study, [111In]In-PNT-DM-HSA and [111In]In-PNT-DA1 showed higher blood retention than [111In]In-PSMA-617. On the other hand, the tumor accumulation of [111In]In-PNT-DA1 was much higher than [111In]In-PNT-DM-HSA and [111In]In-PSMA-617. CONCLUSIONS: These results indicate that the moderate reversible binding of ALB with albumin, not covalent binding, may play a critical role in enhancing the tumor accumulation of PSMA-targeting radioligands.

Synthesis and evaluation of novel trifunctional chelating agents for pretargeting approach using albumin binder to improve tumor accumulation.

INTRODUCTION: The pretargeting approach consists of in vivo ligation between pre-injected antibodies and low-molecular-weight radiolabeled effectors. The advantage of the pretargeting approach is to improve a tumor-to-background ratio, but the disadvantage is to compromise tumor accumulation. In this study, we applied albumin binder (ALB) to the pretargeting approach to overcome low tumor accumulation. METHODS: We synthesized two novel trifunctional effectors containing an ALB moiety, a chelator, and a different tetrazine and two corresponding effectors without an ALB moiety. Albumin-binding assays and stability assays were performed using 111In-labeled effectors. Measurements of reaction rate constant were conducted using 111In-labeled effectors and anti-HER2 antibody trastuzumab modified by trans-cyclooctene, which drives the click reaction with tetrazine. Biodistribution studies using HER2-expressing tumor-bearing mice were performed with or without the pretargeting approach. RESULTS: In albumin-binding assays, ALB-containing effectors exhibited a marked binding to albumin. Two ALB-containing effectors showed the difference in the reactivity and the slight difference in the stability. In biodistribution studies without the pretargeting approach, two ALB-containing effectors showed different pharmacokinetics in blood retention. With the pretargeting approach, the tumor accumulation was improved by the introduction of ALB and the highest tumor accumulation was observed in using the ALB-containing effector with higher blood retention. CONCLUSION: These results suggest that the application of ALB to the pretargeting approach is effective to improve tumor accumulation, and the structure of tetrazine influences the utility of ALB-containing effectors.

Synthesis and biological evaluation of radioiodinated benzoxazole and benzothiazole derivatives for imaging myelin in multiple sclerosis.

Multiple sclerosis (MS) is a chronic inflammatory disease of the central nervous system that results from destruction of the myelin sheath. Due to heterogeneity of the symptoms and course of MS, periodic monitoring of disease activity is important for diagnosis and treatment. In the present study, we synthesized four radioiodinated benzoxazole (BO) and benzothiazole (BT) derivatives, and evaluated their utility as novel myelin imaging probes for single photon emission computed tomography (SPECT). In a biodistribution study using normal mice, three compounds ([125I]BO-1, [125I]BO-2, and [125I]BT-2) displayed moderate brain uptake (2.7, 2.9, and 2.8% ID/g, respectively) at 2 min postinjection. On ex vivo autoradiography using normal mice, [125I]BO-2 showed the most preferable ratio of radioactivity accumulation in white matter (myelin-rich region) versus gray matter (myelin-deficient region). In addition, the radioactivity of [125I]BO-2 was reduced in the lysophosphatidylcholine-induced demyelination region. In conclusion, [123I]BO-2 demonstrated the fundamental characteristics of a myelin imaging probe for SPECT.

In vitro study of the embolic characteristics of imipenem/cilastatin particles.

BACKGROUND: Imipenem/cilastatin (IPM/CS) has long been administered intravenously as a carbapenem antibiotic. However, since this agent is poorly soluble in liquid, occasional reports have described its use as a short-acting, temporary embolic agent. The purpose of this study was to elucidate the characteristics of IPM/CS particles, which are thought to have pain-relieving effects against osteoarthritis-related pain, as an embolic agent. METHODS: Three aspects of IPM/CS as an embolic agent were evaluated in vitro: particle size; particle shape; and change in particle size over time. For particle size, the long diameter was measured. RESULTS: Mean particle size (n=244) was 29.2±12.0 µm (range, 1-60 µm). Shape (n=109) was round in 18.35%, elliptical in 11.93%, and polygonal in 69.72%, showing that most particles were polygonal. In observations of changes in particle size over time (n=9), particles had decreased to 75% of their original size at 82±10.7 min, 50% at 89.3±9.14 min, 25% at 91.3±8.74 min, complete dissolved at 91.8±9.02 min. A rapid shrinkage in diameter was seen in the final period. CONCLUSIONS: IPM/CS particles are ultrafine and the majority display a polygonal shape. This substance shows ultra-short embolic activity. This study revealed the characteristics of a substance that demonstrates an embolic effect not found in existing embolic materials.

Vegetable Extracts as Therapeutic Agents: A Comprehensive Exploration of Anti-Allergic Effects.

Food allergies are common worldwide and have become a major public health concern; more than 220 million people are estimated to suffer from food allergies worldwide. On the other hand, polyphenols, phenolic substances found in plants, have attracted attention for their health-promoting functions, including their anti-allergic effects. In this study, we examined the potential inhibitory effects of 80% ethanol extracts from 22 different vegetables on the degranulation process in RBL-2H3 cells. Our aim was to identify vegetables that could prevent and treat type I allergic diseases. We found strong inhibition of degranulation by extracts of perilla and chives. Furthermore, we verified the respective efficacy via animal experiments, which revealed that the anaphylactic symptoms caused by ovalbumin (OVA) load were alleviated in OVA allergy model mice that ingested vegetable extracts of perilla and chives. These phenomena were suggested to be caused by induction of suppression in the expression of subunits that constitute the high-affinity IgE receptor, particularly the α-chain of FcεR I. Notably, the anti-allergic effects of vegetables that can be consumed daily are expected to result in the discovery of new anti-immediate allergenic drugs based on the components of these vegetables.

Association of Head-Neck Rotation With History of Pitching-Related Elbow Pain in Youth Baseball Players.

Background: Prevention of pitching-related elbow pain in youth baseball players is important. Overhead pitching involves a whole-body motion, including head-neck rotation. A limited range of motion of head-neck rotation may cause inefficient pitching motion; however, this association is unclear. Purpose: To determine whether the range of motion of head-neck rotation is associated with the history of pitching-related elbow pain in youth baseball players. Study Design: Cross-sectional study; Level of evidence, 3. Methods: A total of 311 youth baseball players were selected and asked to complete a questionnaire survey about their age, weight, height, sex, baseball experience, main position, pitching side, and previous/current elbow pain during pitching. The range of motion of the upper and lower limb joints, head-neck rotation, and thoracic kyphosis angle were measured. Binomial logistic regression analysis was used to identify factors associated with the history of elbow pain related to pitching. Results: There were 101 players with a history of pitching-related elbow pain (history group) and 142 players with no pitching-related elbow pain (no-history group). The history group had significantly lower values than the no-history group regarding the range of motion of head-neck rotation on the nondominant side (74.9°± 9° vs 77.7°± 9.6°; P = .02) and overall head-neck rotation (150.6°± 14.7° vs 154.9°± 18.4°; P = .04). Binomial logistic regression analysis identified head-neck rotation on the nondominant side (odds ratio [OR], 0.97 [95% CI, 0.94-1.00]), shoulder horizontal adduction on the dominant side (OR, 0.98 [95% CI, 0.96-1.00]), height (OR, 1.04 [95% CI, 1.00-1.08]), and playing position (pitcher) (OR, 0.40 [95% CI, 0.21-0.76]) as factors associated with a history of pitching-related elbow pain. Conclusion: Our cross-sectional analysis demonstrated that youth baseball players with a history of pitching-related elbow pain had limited head-neck rotation range of motion on the nondominant side, and this was a significant factor associated with the history of pitching-related elbow pain.

Canna Starch Improves Intestinal Barrier Function, Inhibits Allergen Uptake, and Suppresses Anaphylactic Symptoms in Ovalbumin-Induced Food Allergy in Mice.

Edible canna rhizomes contain extremely high levels of resistant starch among cereals and potatoes. We previously showed that feeding canna rhizome starch to mice may increase intestinal barrier function and improve the intestinal environment. Here, we investigated the effects of canna starch intake in a murine food allergy model. Five-week-old female BALB/c mice were divided into four groups: Control and OVA groups fed on the control diet (AIN-93G) ad libitum and Canna and OVA-Canna groups fed on the canna diet (AIN-93G with 10% replaced with canna starch). The OVA and OVA-Canna groups were sensitized to ovalbumin (OVA), and the anaphylactic response was assessed by measuring body temperature. Body temperature was significantly lower in the OVA group than in the non-sensitized group, but no decrease was observed in the OVA-Canna group. Fecal weight, fecal mucin content, and goblet cells of colorectal tissue were significantly increased in the Canna and OVA-Canna groups compared with those in the Control and OVA groups. Allergen uptake into the liver was also increased in the OVA group and decreased in the OVA-Canna group to the same level as in the non-sensitized group. These results indicate that canna starch supplementation in a murine food allergy model suppresses anaphylactic symptoms by improving the intestinal environment and reducing allergen uptake by increasing intestinal barrier function.

Midterm outcomes of transcatheter aortic valve replacement in patients with active cancer.

OBJECTIVES: The clinical outcomes of transcatheter aortic valve replacement (TAVR) in patients with aortic stenosis (AS) and concomitant active cancer remain insufficiently explored. This study aimed to assess the midterm outcomes of TAVR in patients diagnosed with AS and active cancer. METHODS: Data from the OCEAN-TAVI, a prospective Japanese registry of TAVR procedures, was analysed to compare prognoses and clinical outcomes in patients with and without active cancer at the time of TAVR. RESULTS: Of the 2336 patients who underwent TAVR from October 2013 to July 2017, 89 patients (3.8%) had active cancer, whereas 2247 did not. Among patients with active cancer, 49 had limited-stage cancer (stage 1 or 2). The prevalent cancers identified before TAVR were colon (21%), prostate (18%), lung (15%), liver (11%) and breast (9%). Although the periprocedural complications and 30-day mortality rates were comparable between the groups, the 3-year survival rate after TAVR was notably lower in patients with active cancer (64.7%) than in those without active cancer (74.7%; p=0.016). Nevertheless, the 3-year survival rate of patients with limited-stage cancer (stage 1 or 2) did not significantly differ from those without cancer (70.6% vs 74.7%, p=0.50). CONCLUSIONS: The patients with active cancer exhibited significantly reduced midterm survival rates. However, no distinct disparity existed in those with limited-stage cancer (stage 1 or 2). Although TAVR is a viable treatment in patients with AS with active cancer, the type and stage of cancer and prognosis should be carefully weighed in the decision-making process.

Evaluation of Lipopolysaccharide and Interleukin-6 as Useful Screening Tool for Chronic Endometritis.

Universal diagnostic criteria for chronic endometritis (CE) have not been established due to differences in study design among researchers and a lack of typical clinical cases. Lipopolysaccharides (LPSs) have been reported to cause inflammation in the reproductive systems of several animals. This study aimed to elucidate the influence of LPS in the pathogenesis of CE in humans. We investigated whether LPS affected cytokine production and cell proliferation in the endometrium using in vivo and in vitro experiments. LPS concentrations were analyzed between control and CE patients using endometrial tissues. LPS administration stimulated the proliferation of EM-E6/E7 cells derived from human endometrial cells. High LPS concentrations were detected in CE patients. LPS concentration was found to correlate with IL-6 gene expression in the endometrium. Inflammation signaling evoked by LPS led to the onset of CE, since LPS stimulates inflammatory responses and cell cycles in the endometrium. We identified LPS and IL-6 as suitable candidate markers for the diagnosis of CE.

A case of ECPELLA-supported treatment for post-infarction cardiac rupture.

The efficacy and risk of a combination of veno-arterial extracorporeal membrane oxygenation and Impella (Abiomed, Inc., Danvers, MA, USA), an approach known as ECPELLA, for post-infarction cardiac rupture is unclear. We describe the case of a 72-year-old man who presented with acute myocardial infarction. The patient was managed with ECPELLA because of hemodynamic compromise. One week later, there was a sudden increase in venous oxygen saturation. Transthoracic echocardiography revealed ventricular septal rupture, and free wall rupture. Intraventricular thrombus was also observed despite standard anticoagulation therapy. Even with double cardiac rupture, ECPELLA could facilitate left ventricular unloading and sustain hemodynamics. However, because of the risk of device failure due to thrombus aspiration into the Impella, the patient underwent repair surgery. Postoperatively, the patient was temporarily weaned off ECPELLA, and his hemodynamics deteriorated again, and he finally died. Learning objectives: ECPELLA can effectively stabilize the hemodynamics in cases of post-infarction cardiac rupture. However, there are still challenges to address, such as determining optimal ventricular reloading and ECPELLA management for intraventricular thrombus prevention. When using ECPELLA to delay surgery for post-infarction cardiac rupture, it is crucial to strike a balance between hemodynamic stabilization and avoiding potential serious complications.

Synthesis and biological evaluation of novel 18F-labeled 2,4-diaminopyrimidine derivatives for detection of ghrelin receptor in the brain.

The ghrelin receptor (GHSR) is known to regulate various physiological processes including appetite, food intake, and growth hormone release. Its expression is mainly observed in the brain, pancreas, stomach, and intestine. However, the functions of the receptor have not been fully elucidated. GHSR imaging with positron emission tomography (PET) is expected to further understanding of the functions and pathologies of the receptor. In this study, we newly designed and synthesized diaminopyrimidine derivatives ([18F]BPP-1 and [18F]BPP-2) and evaluated their utility as novel PET probes targeting GHSR. In in vitro competitive binding assays, the binding affinity of BPP-2 for GHSR (Ki = 274 nM) was comparable to that of the diaminopyimidine lead compound Abb8a (Ki = 109 nM). In a biodistribution study using normal mice, [18F]BPP-2 displayed low uptake in the brain and moderate uptake in the pancreas, but high radioactivity accumulation in bone was observed due to its defluorination in vivo. Taken together, although further improvement of the pharmacokinetics is needed, the diaminopyrimidine scaffold has potential for the development of useful GHSR-targeting PET probes.